DK0541168T3 - HIV-proteaseinhibitorer, som er egnede til behandling af AIDS - Google Patents

HIV-proteaseinhibitorer, som er egnede til behandling af AIDS

Info

Publication number
DK0541168T3
DK0541168T3 DK92203357.6T DK92203357T DK0541168T3 DK 0541168 T3 DK0541168 T3 DK 0541168T3 DK 92203357 T DK92203357 T DK 92203357T DK 0541168 T3 DK0541168 T3 DK 0541168T3
Authority
DK
Denmark
Prior art keywords
opt
substd
aryl
halo
alkoxy
Prior art date
Application number
DK92203357.6T
Other languages
English (en)
Inventor
Joseph P Vacca
Randall W Hungate
Bruce D Dorsey
M Katharine Holloway
James P Guare
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of DK0541168T3 publication Critical patent/DK0541168T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
DK92203357.6T 1991-11-08 1992-11-02 HIV-proteaseinhibitorer, som er egnede til behandling af AIDS DK0541168T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78950891A 1991-11-08 1991-11-08
US88382592A 1992-05-15 1992-05-15

Publications (1)

Publication Number Publication Date
DK0541168T3 true DK0541168T3 (da) 1998-05-11

Family

ID=27120923

Family Applications (1)

Application Number Title Priority Date Filing Date
DK92203357.6T DK0541168T3 (da) 1991-11-08 1992-11-02 HIV-proteaseinhibitorer, som er egnede til behandling af AIDS

Country Status (27)

Country Link
EP (1) EP0541168B1 (da)
JP (1) JPH0733373B2 (da)
KR (1) KR100273623B1 (da)
AT (1) ATE163926T1 (da)
AU (1) AU659234B2 (da)
BG (1) BG61725B1 (da)
CA (2) CA2195027C (da)
CY (1) CY2090B1 (da)
CZ (1) CZ287610B6 (da)
DE (1) DE69224703T2 (da)
DK (1) DK0541168T3 (da)
ES (1) ES2112880T3 (da)
FI (2) FI106025B (da)
GR (1) GR3026334T3 (da)
HK (1) HK1006060A1 (da)
HU (1) HU220866B1 (da)
IL (1) IL103613A (da)
LV (1) LV12208B (da)
NO (1) NO303383B1 (da)
NZ (1) NZ244986A (da)
PL (1) PL171340B1 (da)
RO (1) RO115726B1 (da)
RU (1) RU2131416C1 (da)
SG (1) SG52731A1 (da)
SK (1) SK281864B6 (da)
UA (1) UA45945C2 (da)
WO (1) WO1993009096A1 (da)

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US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
USH1649H (en) 1987-07-31 1997-05-06 Barrish; Joel C. HIV protease inhibitor combinations
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5888992A (en) 1992-03-11 1999-03-30 Narhex Limited Polar substituted hydrocarbons
DE69333270T2 (de) 1992-03-11 2004-08-05 Narhex Ltd. Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen
US6071895A (en) 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
BR9306058A (pt) * 1992-03-11 1997-11-18 Narhex Ltd Derivados de amina de hidrocarbonetos oxo- e hidroxi- substituidos
US5559256A (en) * 1992-07-20 1996-09-24 E. R. Squibb & Sons, Inc. Aminediol protease inhibitors
ATE218541T1 (de) 1992-08-25 2002-06-15 Searle & Co Hydroxyethylaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
US5430150A (en) * 1992-12-16 1995-07-04 American Cyanamid Company Retroviral protease inhibitors
US5463067A (en) * 1993-07-16 1995-10-31 Merck & Co., Inc. Process for making HIV protease inhibitors
IL110255A (en) * 1993-07-16 1998-12-06 Merck & Co Inc Creation and resolution of 2 tert-butylcarboxamidopiprazine
IL110752A (en) * 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) * 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
IL111584A0 (en) * 1993-11-18 1995-01-24 Merck & Co Inc Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them
US5455351A (en) * 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds
ES2174921T3 (es) * 1993-12-15 2002-11-16 Merck & Co Inc Inhibidores de la proteasa del vih.
US5428167A (en) * 1994-01-14 1995-06-27 American Cyanamid Company Asymmetric synthesis of intermediates for retroviral protease inhibitor compounds
US5733882A (en) * 1994-01-17 1998-03-31 Smithkline Beecham Corporation Retroviral protease inhibitors
TW472047B (en) * 1994-02-04 2002-01-11 Merck & Co Inc Process for making HIV protease inhibitors
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US5728840A (en) * 1994-03-04 1998-03-17 Merck & Co., Inc. Process for making an epoxide
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WO1995029169A2 (de) * 1994-04-20 1995-11-02 Lonza Ag Verfahren zur herstellung von 2-piperazincarbonsäurederivaten
KR100389151B1 (ko) * 1994-04-22 2003-10-04 고에이 가가쿠 고교 가부시키가이샤 광학활성N-tert-부틸-2-피페라진카르복시아미드의제조방법및그라세미화법
UA49803C2 (uk) * 1994-06-03 2002-10-15 Дж.Д. Сьорль Енд Ко Спосіб лікування ретровірусних інфекцій
US5476874A (en) * 1994-06-22 1995-12-19 Merck & Co., Inc. New HIV protease inhibitors
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US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
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US6645961B1 (en) 1997-03-07 2003-11-11 Merck & Co., Inc. Dry granulation formulation for an HIV protease inhibitor
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Also Published As

Publication number Publication date
CA2081970A1 (en) 1993-05-09
CZ111094A3 (en) 1995-03-15
NO303383B1 (no) 1998-07-06
PL171340B1 (pl) 1997-04-30
HU220866B1 (en) 2002-06-29
WO1993009096A1 (en) 1993-05-13
HU9401424D0 (en) 1994-08-29
FI942112A0 (fi) 1994-05-06
FI981591A0 (fi) 1992-11-03
AU2819992A (en) 1993-05-13
FI981591A (fi) 1998-07-10
ATE163926T1 (de) 1998-03-15
SG52731A1 (en) 1998-09-28
FI942112A (fi) 1994-05-06
EP0541168B1 (en) 1998-03-11
SK52394A3 (en) 1995-02-08
LV12208B (en) 1999-03-20
DE69224703T2 (de) 1998-10-15
BG98745A (bg) 1995-03-31
GR3026334T3 (en) 1998-06-30
EP0541168A1 (en) 1993-05-12
NZ244986A (en) 1995-10-26
AU659234B2 (en) 1995-05-11
JPH05279337A (ja) 1993-10-26
IL103613A0 (en) 1993-04-04
CY2090B1 (en) 2002-04-05
IL103613A (en) 1999-05-09
RO115726B1 (ro) 2000-05-30
BG61725B1 (bg) 1998-04-30
NO941696L (da) 1994-06-24
CA2195027A1 (en) 1993-05-09
RU2131416C1 (ru) 1999-06-10
HK1006060A1 (en) 2003-07-10
SK281864B6 (sk) 2001-08-06
LV12208A (lv) 1999-01-20
KR100273623B1 (ko) 2000-12-15
CA2195027C (en) 2000-01-11
FI106025B (fi) 2000-11-15
UA45945C2 (uk) 2002-05-15
HUT70519A (en) 1995-10-30
NO941696D0 (no) 1994-05-06
CA2081970C (en) 1997-07-08
CZ287610B6 (cs) 2001-01-17
DE69224703D1 (de) 1998-04-16
ES2112880T3 (es) 1998-04-16
JPH0733373B2 (ja) 1995-04-12

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